title: Highly efficient intracellular drug delivery with a negatively charged hyperbranched polysulfonamine.
abstract: Efficient intracellular translocation is achieved using an easily prepared hyperbranched polysulfonamine that remains negatively charged at physiological pH. Investigations on the cellular uptake mechanism and the subcellular distribution of PSA are reported. The in vitro cytotoxicity of PSA is found to be low. Using doxorubicin as a model drug, a PSA/drug complex is prepared by electrostatic interaction with a high drug payload that exhibits a controlled release in response to pH. Efficient intracellular drug delivery, strong growth inhibition of tumor cells, and low cytotoxicity to normal cells are observed. The results suggest a possible way to utilize anionic polymers for intracellular delivery of therapeutic moieties or drugs.
authors.affiliation: Department of Nuclear Medicine, Ruijin Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai, China.
authors.forename: Suyun
authors.initials: S
authors.lastname: Chen
authors.forename: Zhonghua
authors.initials: Z
authors.lastname: Tan
authors.forename: Nan
authors.initials: N
authors.lastname: Li
authors.forename: Ruibin
authors.initials: R
authors.lastname: Wang
authors.forename: Lin
authors.initials: L
authors.lastname: He
authors.forename: Yunfeng
authors.initials: Y
authors.lastname: Shi
authors.forename: Lei
authors.initials: L
authors.lastname: Jiang
authors.forename: Peiyong
authors.initials: P
authors.lastname: Li
authors.forename: Xinyuan
authors.initials: X
authors.lastname: Zhu
mesh_terms: D000588:Amines / Q000737:chemistry* / Q000378:metabolism; D000818:Animals; D000838:Anions / Q000737:chemistry; D001692:Biological Transport; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations / Q000138:chemical synthesis* / Q000378:metabolism; D004317:Doxorubicin / Q000737:chemistry / Q000494:pharmacology*; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000378:metabolism; D004705:Endocytosis; D016650:Fluorescein-5-isothiocyanate / Q000032:analysis; D057809:HEK293 Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D051379:Mice; D041681:NIH 3T3 Cells; D009369:Neoplasms / Q000188:drug therapy; D011108:Polymers / Q000737:chemistry* / Q000378:metabolism; D055672:Static Electricity; D013450:Sulfones / Q000737:chemistry* / Q000378:metabolism
chemical_list: D000588:Amines; D000838:Anions; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D011108:Polymers; D013450:Sulfones; C017662:polysulfone P 1700; D004317:Doxorubicin; D016650:Fluorescein-5-isothiocyanate